Description
Cimetropium Bromide (DA-3177) is a mAChR antagonist for long-term treatment of irritable bowel syndrome.
Product information
CAS Number: 51598-60-8
Molecular Weight: 438.36
Formula: C21H28BrNO4
Chemical Name: (1R,2R,4S,5S,7S)-9-(cyclopropylmethyl)-7-{[(2S)-3-hydroxy-2-phenylpropanoyl]oxy}-9-methyl-3-oxa-9-azatricyclo[3.3.1.0²,⁴]nonan-9-ium bromide
Smiles: [Br-].C[N+]1(CC2CC2)[C@@H]2C[C@H](C[C@H]1[C@@H]1O[C@@H]12)OC(=O)[C@H](CO)C1C=CC=CC=1
InChiKey: WDURTRGFUGAJHA-GSWUYBTGSA-M
InChi: InChI=1S/C21H28NO4.BrH/c1-22(11-13-7-8-13)17-9-15(10-18(22)20-19(17)26-20)25-21(24)16(12-23)14-5-3-2-4-6-14;/h2-6,13,15-20,23H,7-12H2,1H3;1H/q+1;/p-1/t15-,16-,17-,18+,19-,20+,22?;/m1./s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: H2O : 50 mg/mL (114.06 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Cimetropium Bromide behaves as a competitive antagonist of muscarinic-mediated contractions in isolated colonic preparations from both species, with affinity values (pA2) ranging between 7.41 and 7.82. Cimetropium has potent antimuscarinic effect in inhibition of contraction of longitudinal muscle preparations. In the superfusion experiments of the preparation which has been preloaded with labelled choline, Cimetropium decreases the labelled ACh release induced by electrical field stimulation under the muscarinic autoinhibition blocked-condition.
In Vivo:
When administered intravenously to conscious dogs provided with a colonic Thiry fistula, Cimetropium is a potent inhibitor of large bowel motility evoked by both exogenous and endogenous stimuli. Cimetropium Bromide (10-100 μg/kg) counteracts colonic motor response to neostigmine administration with an ID50 of 27.9 μg/kg; both tonic and phasic components of contractile response are affected. In a comparable range of doses (3-100μg/kg), the drug inhibits motor activity elicited by intraluminal distension.
Products are for research use only. Not for human use.
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